Haffmans J, Dzoljic M R
Pharmacology. 1987;34(2-3):61-5. doi: 10.1159/000138253.
We examined the effect of opioid receptor antagonists on the seizure phenomena induced by specific delta opioid receptor agonist [D-Ser2,Leu5] enkephalyl-Thr (DSLET). The experiments have been performed in the anesthetized rats, and the DSLET-induced seizure phenomena were registered by electrocorticogram and electromyogram. It was demonstrated that two selective delta opioid receptor antagonists, ICI 152,129 and ICI 174,864 inhibited DSLET-induced epileptiform ECoG pattern and myoclonic contractions in a dose-related manner. An equimolar concentration of naloxone failed to antagonize the epileptiform effects of DSLET. It is concluded that delta opioid receptor agonist-induced seizure is mediated by delta receptors, since it can be blocked by delta opioid receptor antagonists. Evidently, delta opioid antagonists can be used as a good tool, in order to demonstrate a delta component in the seizure phenomena induced by other endogenous opioid peptides or their derivatives.
我们研究了阿片受体拮抗剂对由特异性δ阿片受体激动剂[D-丝氨酸2,亮氨酸5]脑啡肽-苏氨酸(DSLET)诱导的癫痫发作现象的影响。实验在麻醉大鼠中进行,通过脑电图和肌电图记录DSLET诱导的癫痫发作现象。结果表明,两种选择性δ阿片受体拮抗剂ICI 152,129和ICI 174,864以剂量相关的方式抑制了DSLET诱导的癫痫样脑电图模式和肌阵挛收缩。等摩尔浓度的纳洛酮未能拮抗DSLET的癫痫样作用。结论是,δ阿片受体激动剂诱导的癫痫发作是由δ受体介导的,因为它可被δ阿片受体拮抗剂阻断。显然,δ阿片拮抗剂可作为一种很好的工具,用于证明由其他内源性阿片肽或其衍生物诱导的癫痫发作现象中的δ成分。